Statins (HMG-CoA reductase inhibitors) are a group of highly efficient pharmacological agents used for reducing blood cholesterol level and prevention/treatment of cardiovascular disease. Adverse reactions during statin treatment affect quite significant numbers of patients (reportedly from 5% to 20%), with more side effects occurring at higher doses. Reduced statin dosing can be achieved by improved bioavailability of statins, which is fairly low due to poor aqueous solubility, low permeability and high molecular weight of some members of the statin family. Moreover, since hepatic cholesterologenesis is a main target of statin action and extrahepatic inhibition of HMG-CoA reductase has no effect on plasma lipids, hepatic bioavailability, in our opinion, becomes a new important modality of statins maximizing their potential effect on the plasma lipid profile and diminishing their extrahepatic toxicity. Therefore efficient delivery systems of statins into hepatocytes need to be developed and introduced. Uses of nano-emulsifying statin delivery systems which may include vectors of intrahepatic transport, in particular lycopene, are discussed. As a proof of concept, some preliminary results revealing the effect of a lycopene-containing nanoformulation of simvastatin (designated as Lyco-Simvastatin) on LDL in mildly hypercholesterolemic patients are shown.